EZH2

EZH2-IN-13, a potent EZH2 inhibitor, exhibits potential anticancer activity and may be utilized to study diseases associated with EZH2 activity.

EZH2-IN-15 (SHR2554) is a specific inhibitor of the zeste 2 histone modification enhancer (EZH2).EZH2 is aberrantly overexpressed in many human cancers and controls adaptive responses by regulating Treg activity. EZH2 expression in tumors has also been shown to control innate immunity.

Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma/follicular lymphoma.

3-Deazaneplanocin A HCl is a synthetically derived inhibitor of the histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (SAHH). By regulating epigenetic methylation pathways, 3-deazaneplanocin A induces apoptosis and inhibits tumor cell proliferation, demonstrating significant antitumor activity in various tumor models. 3-deazaneplanocin A HCl can be used in research on epigenetic regulation, tumorigenesis and progression, and stem cell differentiation.

Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).

ZLD1039 is a potent, orally bioavailable EZH2 (Enhancer of Zeste Homolog 2) inhibitor with high selectivity. It demonstrates strong, concentration-dependent inhibition of both wild-type and mutant (Y641F and A677G) PRC2 (Polycomb Repressive Complex 2) enzymatic activities, exhibiting IC50 values of 5.6, 15, and 4.0 nM, respectively. Additionally, ZLD1039 effectively suppresses breast tumor growth and metastasis.

CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.

(S)-HH2853 is a potent dual inhibitor of EZH1 and EZH2, inhibiting EZH2_Y641F with an IC50 of <100 nM.(S)-HH2853 has potential antitumor activity and can be used in the study of autoimmune diseases.

(R)-HH2853 is a potent EZH2 inhibitor with an IC50 <100 nM for EZH2-Y641F.(R)-HH2853 has anticancer and antitumor activity and can be used in autoimmune diseases.

(2R,4S)-Azalanstat (Iso-Azalansta) is a selective heme oxygenase (HO) inhibitor that is used in the study of cardiovascular disease.

EPZ011989 is a effective, specific orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 Y646 and EZH2 wt; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.

GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM.

PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 (Kis: 0.7 and 3.0 nM, respectively).

Valemetostat (DS-3201) is an EZH1/2 inhibitor that can be used to study relapsed/refractory peripheral T-cell lymphoma.

MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).

EBI-2511 is a highly potent, orally active inhibitor of EZH2, with an IC50 of 6 nM in Pfeffiera cell lines.

Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleo

NSC745885 is an antitumor agent non-toxic to normal cells that downregulates EZH2 via proteasome-mediated degradation. It exhibits toxicity against multiple normal and drug-resistant cancer cell lines and may be used in studies of advanced bladder cancer and oral squamous cell carcinoma.

GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.

EPZ005687, a potent and selective inhibitor of EZH2.

GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).

UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).

Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor with antitumor activity, utilized in the study of ovarian cancer and advanced solid tumors.

GSK343, a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against other histone methyltransferases.